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2. 发明申请

WO2005103018A1 UREA DERIVATIVES AS ANTAGONISTS OF THE VANILLOID RECEPTOR (VR1) 审中-公开
标题翻译：尿素衍生物作为VANILLOID受体（VR1）的拮抗剂
公开(公告)号：WO2005103018A1
公开(公告)日：2005-11-03
申请号：PCT/EP2005/003632
申请日：2005-04-07
申请人： BAYER HEALTHCARE AG , FUJISHIMA, Hiroshi , MOGI, Muneto , YUASA, Hiroaki , TAIJIMI, Masaomi , YAMAMOTO, Noriyuki , HAYASHI, Fumihiko , TSUKIMI, Yasuhiro , GUPTA, Jang
发明人： FUJISHIMA, Hiroshi , MOGI, Muneto , YUASA, Hiroaki , TAIJIMI, Masaomi , YAMAMOTO, Noriyuki , HAYASHI, Fumihiko , TSUKIMI, Yasuhiro , GUPTA, Jang
IPC分类号： C07D265/36
CPC分类号： C07D265/36 , C07D215/227
摘要： This invention relates to urea derivatives according to general formula I and salts thereof which are useful as active ingredients of pharmaceutical preparations. The urea derivatives of the present invention have an excellent activity as VR1 antagonists and are useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urological disorder or disease, such as detrusor overactivity (overactive bladder), urinary incontinence, neurogenic detrusor oeractivity (detrusor hyperflexia), idiopathic detrusor overactivity (detrusor instability), benign prostatic hyperplasia, and lower urinary tract symptoms; chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke; and respiratory diseases and inflammatory disorders such as asthma, chronic obstructive pulmonary (or airways) disease (COPD), common cold, cough, sneeze, bronchitis including acute and chronic bronchitis, bronchiolitis, rhinitis, allergic rhinitis, vasomotor rhinitis, mucositis, sinusitis, allergy, disorders associated with exogenous irritants such as tobacco smoke, smog, high levels of atmospheric SO2 and noxious gases in the workplace, and airways hyperreactivity, milk product intolerance, Loffler's pneumonia, emphysema, cystic fibrosis, bronchiectasis, pulmonary fibrosis, pneumoconiosis, collagen vascular disease, granulomatous disease, laryngitis, pharyngitis, pneumonia, pleuritis, persistent asthma and chronic asthmatic bronchitis. Formula I Wherein n represents 0, 1, 2, 3, or 4; X represents O, CH 2 , S, or N(R 10 ), Wherein R 10 respresents hydrogen or C 1-6 alkyl
摘要翻译：本发明涉及可用作药物制剂活性成分的通式Ⅰ的脲衍生物及其盐。本发明的尿素衍生物作为VR1拮抗剂具有优异的活性，并且可用于预防和治疗与VR1活性有关的疾病，特别是用于治疗泌尿系统疾病或疾病，例如逼尿肌过度活动症（膀胱过度活动症），尿失禁，神经源性逼尿肌反应性（逼尿肌hyperflexia），特发性逼尿肌过度活动（逼尿肌不稳定），良性前列腺增生和下尿路症状; 慢性疼痛，神经性疼痛，术后疼痛，类风湿关节炎疼痛，神经痛，神经病，痛觉，神经损伤，局部缺血，神经退行性卒中; 呼吸系统疾病和哮喘，慢性阻塞性肺（或气道）疾病（COPD），感冒，咳嗽，打喷嚏，支气管炎，包括急性和慢性支气管炎，细支气管炎，鼻炎，过敏性鼻炎，血管舒缩性鼻炎，粘膜炎，鼻窦炎，过敏，与外来刺激物如烟草烟雾，烟雾，工作场所大气中二氧化硫和有毒气体高度相关的疾病，气道高反应性，乳制品不耐受，霍夫勒氏肺炎，肺气肿，囊性纤维化，支气管扩张，肺纤维化，肺尘埃沉着病，胶原蛋白血管疾病，肉芽肿病，喉炎，咽炎，肺炎，胸膜炎，持续性哮喘和慢性哮喘性支气管炎。其中n表示0,1,2,3或4; X表示O，CH 2，S或N（R 10），其中R 10表示氢或C 1-6烷基

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